详情描述
Galiellalactone is a is a small non-toxic and non-mutagenic fungal metabolite, a selective inhibitor of STAT3 signaling, with an IC50 of 250-500 nM. Galiellalactone can be used to research castration-resistant prostate cancer.
Product information
CAS Number: 133613-71-5
Molecular Weight: 194.23
Formula: C11H14O3
Chemical Name: (4R, 7R, 9S, 11S)-11-hydroxy-9-methyl-3-oxatricyclo[5.3.1.0, ]undec-1(10)-en-2-one
Smiles: C[C@H]1C[C@H]2CC[C@H]3OC(=O)C(=C1)[C@@]23O
InChiKey: SOIISBQQYAGDKM-QJSROADHSA-N
InChi: InChI=1S/C11H14O3/c1-6-4-7-2-3-9-11(7,13)8(5-6)10(12)14-9/h5-7,9,13H,2-4H2,1H3/t6-,7+,9+,11-/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Galiellalactone (2.5-25 μM; 24-72 hour) induces apoptosis of prostate cancer (PCa) cell lines expressingp-Stat3. Galiellalactone (2.5-25 μM; 24-72 hour) decreases viability of DU145 cells. Galiellalactone (10 μM) inhibits STAT3 signaling activity as assessed by luciferase reporter gene assay in IL-6-stimulated LNCaP cells. Galiellalactone (10-100 μM; 1 hour) binds directly to STAT3 in DU145 cells. Galiellalactone (5-50 μM; 1 hour) interferes with STAT3 DNA binding without inhibiting phosphorylation in DU145 cells.
In Vivo:
Galiellalactone (1, 3 mg/kg; daily i.p. for 3 weeks) inhibits PCa tumor growth in vivo.
References:
- Hellsten R, et, al. Galiellalactone is a novel therapeutic candidate against hormone-refractory prostate cancer expressing activated Stat3. Prostate. 2008 Feb 15; 68(3): 269-80.
- Doncow DN, et, al. Galiellalactone is a direct inhibitor of the transcription factor STAT3 in prostate cancer cells. J Biol Chem. 2014 Jun 6; 289(23): 15969-78.
- Weidler M, et, al. Inhibition of interleukin-6 signaling by galiellalactone. FEBS Lett. 2000 Oct 27; 484(1): 1-6.
Products are for research use only. Not for human use.